Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model
Parkinson's disease is a neurodegenerative disorder that requires treatment by dopaminergic agonists, which may be responsible for central side effects. We hypothesized that the efflux transporter ABCB1/P-glycoprotein played a role in brain disposition of antiparkinsonian drugs and could contro...
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| المؤلف الرئيسي: | |
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| مؤلفون آخرون: | , , , , |
| التنسيق: | article |
| منشور في: |
2008
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| الوصول للمادة أونلاين: | http://hdl.handle.net/10725/4499 http://dx.doi.org/10.1016/j.neulet.2008.06.055 http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php http://www.sciencedirect.com/science/article/pii/S0304394008008793 |
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| _version_ | 1864513463686004736 |
|---|---|
| author | Vautier, Sarah |
| author2 | Milane, Aline Fernandez, Christine Buyse, Marion Chacun, Helene Farinotti, Robert |
| author2_role | author author author author author |
| author_facet | Vautier, Sarah Milane, Aline Fernandez, Christine Buyse, Marion Chacun, Helene Farinotti, Robert |
| author_role | author |
| dc.creator.none.fl_str_mv | Vautier, Sarah Milane, Aline Fernandez, Christine Buyse, Marion Chacun, Helene Farinotti, Robert |
| dc.date.none.fl_str_mv | 2008 2016-10-04T09:56:39Z 2016-10-04T09:56:39Z 2016-10-04 |
| dc.identifier.none.fl_str_mv | 0304-3940 http://hdl.handle.net/10725/4499 http://dx.doi.org/10.1016/j.neulet.2008.06.055 Vautier, S., Milane, A., Fernandez, C., Buyse, M., Chacun, H., & Farinotti, R. (2008). Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model. Neuroscience letters, 442(1), 19-23. http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php http://www.sciencedirect.com/science/article/pii/S0304394008008793 |
| dc.language.none.fl_str_mv | en |
| dc.relation.none.fl_str_mv | Neuroscience Letters |
| dc.rights.*.fl_str_mv | info:eu-repo/semantics/openAccess |
| dc.title.none.fl_str_mv | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model |
| dc.type.none.fl_str_mv | Article info:eu-repo/semantics/publishedVersion info:eu-repo/semantics/article |
| description | Parkinson's disease is a neurodegenerative disorder that requires treatment by dopaminergic agonists, which may be responsible for central side effects. We hypothesized that the efflux transporter ABCB1/P-glycoprotein played a role in brain disposition of antiparkinsonian drugs and could control central toxicity. We aimed to evaluate antiparkinsonian drugs as ABCB1 substrates and/or inhibitors in rat brain endothelial cells GPNT, in order to predict potential clinical drug–drug interactions. Among the antiparkinsonian drugs tested, levodopa, bromocriptine, pergolide and pramipexole were ABCB1 substrates. However, only bromocriptine could inhibit ABCB1 functionality with an IC50 of 6.71 μM on Rhodamine 123 uptake and an IC50 of 1.71 μM on digoxine uptake. Thus, bromocriptine at 100 μM is responsible for an increase of levodopa intracellular transport of about 2.05-fold versus control. Therefore, we can conclude that bromocriptine is a potent drug for medicinal interactions in vitro. Hence, in patients with Parkinson's disease, these results may be considered to optimise treatments individually. |
| eu_rights_str_mv | openAccess |
| format | article |
| id | LAURepo_8fb6bceb0f22ad35a4fd4d1864c586b7 |
| identifier_str_mv | 0304-3940 Vautier, S., Milane, A., Fernandez, C., Buyse, M., Chacun, H., & Farinotti, R. (2008). Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model. Neuroscience letters, 442(1), 19-23. |
| language_invalid_str_mv | en |
| network_acronym_str | LAURepo |
| network_name_str | Lebanese American University repository |
| oai_identifier_str | oai:laur.lau.edu.lb:10725/4499 |
| publishDate | 2008 |
| repository.mail.fl_str_mv | |
| repository.name.fl_str_mv | |
| repository_id_str | |
| spelling | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell modelVautier, SarahMilane, AlineFernandez, ChristineBuyse, MarionChacun, HeleneFarinotti, RobertParkinson's disease is a neurodegenerative disorder that requires treatment by dopaminergic agonists, which may be responsible for central side effects. We hypothesized that the efflux transporter ABCB1/P-glycoprotein played a role in brain disposition of antiparkinsonian drugs and could control central toxicity. We aimed to evaluate antiparkinsonian drugs as ABCB1 substrates and/or inhibitors in rat brain endothelial cells GPNT, in order to predict potential clinical drug–drug interactions. Among the antiparkinsonian drugs tested, levodopa, bromocriptine, pergolide and pramipexole were ABCB1 substrates. However, only bromocriptine could inhibit ABCB1 functionality with an IC50 of 6.71 μM on Rhodamine 123 uptake and an IC50 of 1.71 μM on digoxine uptake. Thus, bromocriptine at 100 μM is responsible for an increase of levodopa intracellular transport of about 2.05-fold versus control. Therefore, we can conclude that bromocriptine is a potent drug for medicinal interactions in vitro. Hence, in patients with Parkinson's disease, these results may be considered to optimise treatments individually.PublishedN/A2016-10-04T09:56:39Z2016-10-04T09:56:39Z20082016-10-04Articleinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article0304-3940http://hdl.handle.net/10725/4499http://dx.doi.org/10.1016/j.neulet.2008.06.055Vautier, S., Milane, A., Fernandez, C., Buyse, M., Chacun, H., & Farinotti, R. (2008). Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model. Neuroscience letters, 442(1), 19-23.http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.phphttp://www.sciencedirect.com/science/article/pii/S0304394008008793enNeuroscience Lettersinfo:eu-repo/semantics/openAccessoai:laur.lau.edu.lb:10725/44992021-03-19T10:00:50Z |
| spellingShingle | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model Vautier, Sarah |
| status_str | publishedVersion |
| title | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model |
| title_full | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model |
| title_fullStr | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model |
| title_full_unstemmed | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model |
| title_short | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model |
| title_sort | Interactions between antiparkinsonian drugs and ABCB1/P-glycoprotein at the blood–brain barrier in a rat brain endothelial cell model |
| url | http://hdl.handle.net/10725/4499 http://dx.doi.org/10.1016/j.neulet.2008.06.055 http://libraries.lau.edu.lb/research/laur/terms-of-use/articles.php http://www.sciencedirect.com/science/article/pii/S0304394008008793 |